RRC ID 67246
著者 Togami K, Miyao A, Miyakoshi K, Kanehira Y, Tada H, Chono S.
タイトル Efficient delivery to human lung fibroblasts (WI-38) of pirfenidone incorporated into liposomes modified with truncated basic fibroblast growth factor and its inhibitory effect on collagen synthesis in idiopathic pulmonary fibrosis.
ジャーナル Biol Pharm Bull
Abstract In the present in vitro study, we assessed the delivery of pirfenidone incorporated into liposomes modified with truncated basic fibroblast growth factor (tbFGF) to lung fibroblasts and investigated the anti-fibrotic effect of the drug. The tbFGF peptide, KRTGQYKLC, was used to modify the surface of liposomes (tbFGF-liposomes). We used the thin-layer evaporation method, followed by sonication, to prepare tbFGF-liposomes containing pirfenidone. The cellular accumulation of tbFGF-liposomes was 1.7-fold greater than that of non-modified liposomes in WI-38 cells used as a model of lung fibroblasts. Confocal laser scanning microscopy showed that tbFGF-liposomes were widely localized in WI-38 cells. The inhibitory effects of pirfenidone incorporated into tbFGF-liposomes on transforming growth factor-β1 (TGF-β1)-induced collagen synthesis in WI-38 cells were evaluated by measuring the level of intracellular hydroxyproline, a major component of the protein collagen. Pirfenidone incorporated into tbFGF-liposomes at concentrations of 10, 30, and 100 µM significantly decreased the TGF-β1-induced hydroxyproline content in WI-38 cells. The anti-fibrotic effect of pirfenidone incorporated into tbFGF-liposomes was enhanced compared with that of pirfenidone solution. These results indicate that tbFGF-liposomes are a useful drug delivery system of anti-fibrotic drugs to lung fibroblasts for the treatment of idiopathic pulmonary fibrosis.
巻・号 38(2)
ページ 270-6
公開日 2015-1-1
DOI 10.1248/bpb.b14-00659
PMID 25747986
MeSH Cell Line Cell Proliferation / drug effects Collagen / metabolism Fibroblast Growth Factors / administration & dosage* Fibroblast Growth Factors / chemistry* Fibroblasts / drug effects* Fibroblasts / metabolism HEK293 Cells Humans Idiopathic Pulmonary Fibrosis / drug therapy Idiopathic Pulmonary Fibrosis / metabolism Liposomes Lung / cytology Pyridones / administration & dosage*
IF 1.863
リソース情報
ヒト・動物細胞 293(RCB1637) WI-38(RCB0702)